Fedratinib (SAR302503, TG101348)
商品编号:
TS0101
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详细介绍
l 基本信息 |
产品名称 | Fedratinib (SAR302503, TG101348) |
一般描述 | Fedratinib is a selective inhibitor of JAK2. |
别 称 | N-tert-butyl-3-[[5-methyl-2-[4-(2-pyrrolidin-1-ylethoxy)anilino]pyrimidin-4-yl]amino]benzenesulfonamide |
纯 度 | ≥98.0%(HPLC) | CAS NO. | 936091-26-8 |
分子式 | C27H36N6O3S | 分子量 | 524.68 |
适用范围 | 生物试剂,适用于细胞培养等 |
l 理化信息 |
外 观 | 固体 |
溶解性(25℃) | DMSO | ≥50mg/mL |
乙醇 | Insoluble |
水 | Insoluble |
l 生物学信息 |
生物活性/药理作用 | Fedratinib is an orally bioavailable, small-molecule, ATP-competitive inhibitor of Janus-associated kinase 2 (JAK2)
with potential antineoplastic activity. Fedratinib competes with JAK2 as well as the mutated form AK2V617F for ATP binding, which may result in inhibition of JAK2 activation, inhibition of the JAK-STAT signaling pathway, and the induction of tumor cell apoptosis. JAK2 is the most common mutated gene in bcr-abl-negative myeloproliferative disorders (MPDs); the mutated form JAK2V617F has a valine-to-phenylalanine modification at position 617 and plays a key role in tumor cell proliferation and survival. Fedratinib is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. |
l 存储 |
存储温度 | -20℃ |
l 注意事项及免责声明 |
本产品仅用于实验研究,不得作为药物使用,不得用于家用或其它用途。 |
l 参考文献 |
1. http://www.drugbank.ca 2. https://ncit.nci.nih.gov 3. https://www.ncbi.nlm.nih.gov |